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Fibrous surface structure containing active ingredients with controlled release of active ingredients, use thereof and method for the production thereof

a technology of fibrous and surface structure, which is applied in the field of fibrous surface structure containing, can solve the problems of controlling the release of formulated active ingredients, and achieve the effect of reducing the risk of cancer and affecting the survival rate of cancer patients

Inactive Publication Date: 2011-06-02
BASF AG
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

[0014]It was therefore an object of the present invention to provide a process which allows the formulation of such active ingredients using polymer materials as formulating aids, while enabling better adjustment of the active ingredient release than is known from the prior art.

Problems solved by technology

Especially the control of the release of the formulated active ingredients, for example over prolonged periods, constitutes a problem which is yet to be solved satisfactorily to date.

Method used

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  • Fibrous surface structure containing active ingredients with controlled release of active ingredients, use thereof and method for the production thereof
  • Fibrous surface structure containing active ingredients with controlled release of active ingredients, use thereof and method for the production thereof
  • Fibrous surface structure containing active ingredients with controlled release of active ingredients, use thereof and method for the production thereof

Examples

Experimental program
Comparison scheme
Effect test

example 1

Production and Properties of the Composite Fibers from PVP and Epoxiconazole

[0322]To produce composite fibers, polymer solutions were produced from poly(1-vinyl-2-pyrrolidinone) Kollidon K-90 (PVP) (Mw=1 100 000 g / mol, Tg=180° C., BASF SE) and epoxiconazole fungicide (1-{[3-(2-chlorophenyl)-2-(4-fluorophenyl)oxiran-2-yl]methyl}-1H-1,2,4-triazole) in an ethanol / water mixture (90:10) and spun to fibers. This involves spinning the solutions with a spinning system under voltages between 35 and 45 kV.

[0323]The starting weights are listed in the following table:

Activeingredientcontent, % byMaterialMass, gweightEthanol7.104Water0.998PVP0.486Epoxiconazole0.04869.1″0.097216.7″0.14623.1″0.19428.6″0.24333.3

The concentration figures of the epoxiconazole active ingredient are based on total solids (PVP+active ingredient). The concentration of the carrier polymer is based on the total mass of solvent and polymer before the addition of the active ingredient.

[0324]FIG. 1A shows the fiber morphology...

example 2

Production and Properties of the Composite Fibers Formed by PVP and Beta-carotene.

[0333]β-Carotene is used to color fatty foods such as butter, margarine, cheese, mayonnaise and—in water-dispersible form—also water-containing foods, for example fruit drinks, puddings, confectionary. β-carotene is also used as a dye for cosmetics and as an animal feed additive. To produce composite fibers, polymer solutions were produced from poly(1-vinyl-2-pyrrolidinone) Kollidon K-90 (PVP) (Mw=1 100 000 g / mol, Tg=180° C., BASF SE) and the β-carotene dye in chloroform and spun to fibers. For this purpose, the solutions were spun with a syringe system under voltages between 40 and 45 kV. In addition, 0.5% by weight, based on the overall formulation, of benzyltributylammonium bromide was added thereto in order to increase the electrical conductivity of the solution. This has a positive effect on the fiber morphology and diameter distribution: fewer beads form and the fiber diameter distribution become...

example 3

Production and Properties of the Composite Fibers Formed by PMMA and Epoxiconazole

[0345]In order to further illustrate the broad applicability of the method, composite fibers were produced from poly(methyl methacrylate) and epoxiconazole fungicide.

[0346]To produce composite fibers, polymer solutions were produced from poly(methyl methacrylate) Plexiglas® (PMMA) (Mw=430 000 g / mol, Tg=110° C. (Iso 11357)) and epoxiconazole fungicide (1-{[3-(2-chlorophenyl)-2-(4-fluorophenyl)oxiran-2-yl]methyl}-1H-1,2,4-triazole) in an ethanol / chloroform mixture (6:11) and spun to fibers. For this purpose, the solutions were spun with a syringe system under voltages between 40 and 45 kV.

[0347]The starting weights are listed in the following table:

Active ingredientcontent, % byMaterialMass, gweightEthanol5.53Chloroform10.14PMMA1.00Epoxiconazole0.1110″0.2520″0.4330″1.0050

[0348]The concentration figures for the epoxiconazole active ingredient are based on total solids (PMMA+active ingredient). The concent...

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Abstract

The invention relates to a fibrous surface structure containing active ingredients with an adjustable active ingredient release profile, comprising a fibrous, polymeric, soluble and / or degradable active ingredient substrate and at least one active ingredient that is associated with the substrate and can be released by the fibrous surface structure; to formulations containing active ingredients, comprising such fibrous surface structures; to the use of fibrous surface structures containing active ingredients according to the invention for producing formulations containing active ingredients; and to a method for producing fibrous surface structures according to the invention.

Description

[0001]The invention relates to active ingredient-containing fibrous sheetlike structures with an adjustable active ingredient release profile, comprising a fibrous, polymeric, soluble and / or degradable active ingredient carrier and at least one active ingredient which is associated with the carrier and can be released by the fibrous sheetlike structure; to active ingredient-containing formulations comprising such fibrous sheetlike structures; to the use of inventive active ingredient-containing fibrous sheetlike structures for production of active ingredient-containing formulations; and to processes for production of inventive fibrous sheetlike structures.STATE OF THE ART[0002]For production of nano- and mesofibers, the person skilled in the art is aware of a multitude of processes, among which electrospinning is currently of the greatest significance. In this process, which is described, for example, by D. H. Reneker, H. D. Chun in Nanotechn. 7 (1996), pages 216 ff., a polymer melt...

Claims

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Application Information

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IPC IPC(8): A61K9/70A61K47/32A61K47/30A61K8/72A01N25/00A61K8/02A01P3/00A23P1/10A23L1/308A23K1/16D04H1/42D04H1/728
CPCA61K9/70A61K31/4174C07K14/43518A61K47/32A61K47/42A61K31/4196A61P31/10
Inventor LIEBMANN, BURGHARDKLIMOV, EVGUENI
Owner BASF AG
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